Department of Anesthesiology, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, China.
Drug Deliv. 2021 Dec;28(1):1080-1092. doi: 10.1080/10717544.2021.1931558.
The principal goal of the present investigation was to enterprise new and effective drug delivery vesicle for the sustained delivery of local anesthetic lidocaine hydrochloride (LDC), using a novel combination of copolymeric hydrogel with tetrahydroxyborate (COP-THB) to improve bioactivity and therapeutic potential. To support this contention, the physical and mechanical properties, rheological characteristics, and component release of candidate formulations were investigated. An optimized formulation of COP-THB containing LDC to an upper maximum concentration of 1.5% w/w was assessed for drug crystallization. The biocompatibility of the prepared COP-THB hydrogel was exhibited strong cell survival (96%) and growth compatibility on L929 fibroblast cell lines, which was confirmed by using methods of MTT assay and microscopic observations. The COP-THB hydrogel release pattern is distinct from that of COP-THB/LDC hydrogels by the slow-release rate and the low percentage of cumulative release. evaluations were demonstrated the anesthetic effects and toxicity value of treated samples by using mice models. In addition, COP-THB/LDC hydrogels significantly inhibit in vivo tumor growth in mice model and effectively reduced it is toxicity. The pharmacological evaluation showed that encapsulation of LDC in COP-THB hydrogels prolonged its anesthetic action with favorable and compatibility. This novel design may theoretically be used in promising studies involving the controlled release of local anesthetics.HighlightsDevelopment a modified sustained release system for the local anesthetic lidocaine.PVP-THB hydrogel to improve the pharmacological properties of the drug and their anesthetic activities.Profiles of PVP-THB/LDC showed that the effective release of associated lidocaine.This new formulation could potentially be used in future local anesthetics.
本研究的主要目的是开发新的有效的药物传递囊泡,以持续传递局部麻醉药盐酸利多卡因(LDC),使用四羟基硼酸盐(COP-THB)的新型共聚水凝胶来提高生物活性和治疗潜力。为了支持这一论点,对候选配方的物理和机械性能、流变特性和成分释放进行了研究。评估了含有 LDC 的 COP-THB 的优化配方,其最高浓度可达 1.5%w/w,以评估药物结晶。通过 MTT 测定和显微镜观察证实,所制备的 COP-THB 水凝胶具有很强的细胞存活率(96%)和生长相容性。COP-THB 水凝胶的释放模式与 COP-THB/LDC 水凝胶明显不同,其释放速度较慢,累积释放百分比较低。通过小鼠模型评估了处理样品的麻醉效果和毒性值。此外,COP-THB/LDC 水凝胶显著抑制了小鼠模型中的体内肿瘤生长,并有效降低了其毒性。药理评价表明,将 LDC 包封在 COP-THB 水凝胶中延长了其麻醉作用,具有良好的和相容性。这种新设计理论上可用于涉及局部麻醉剂控释的有前途的研究。
亮点
为局部麻醉剂利多卡因开发改良的持续释放系统。
PVP-THB 水凝胶可改善药物的药理学特性及其麻醉活性。
PVP-THB/LDC 的特性表明相关利多卡因的有效释放。
这种新配方将来可能用于局部麻醉剂。